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Found 2 translations.
| Name | Current message text |
|---|---|
| h English (en) | In the early 1980s it was noted that a series of imidazole-5-[[acetic acid]] [[Derivative (chemistry)|derivatives]] diminished blood pressure responses to Ang II in rats. Two compounds, [[S-8307]] and [[S-8308]], were later found to be highly specific and promising non-peptide Ang II receptor antagonists but using [[molecular modeling]] it was seen that their structures would have to [[mimic]] more closely the [[pharmacophore]] of Ang II. Structural modifications were made and the orally active, potent and [[Ligand (biochemistry)#Selective and non-selective|selective]] nonpeptide AT<sub>1</sub> receptor blocker [[losartan]] was developed. In 1995 losartan was approved for clinical use in the United States and since then six additional ARBs have been approved. These drugs are known for their excellent [[Adverse effect (medicine)|side-effects]] profiles, which [[clinical trials]] have shown to be similar to those of [[placebos]]. |
| h Japanese (ja) | 1980年代初頭、一連のイミダゾール-5-[[acetic acid/ja|酢酸]]がラットのAng IIに対する血圧応答を低下させることが注目された。[[Derivative (chemistry)/ja|誘導体]]がラットのAng IIに対する血圧応答を低下させることが1980年代に注目された。[[S-8307/ja|S-8307]]と[[S-8308/ja|S-8308]]の2つの化合物は、後に非常に特異的で有望な非ペプチド性のAng II受容体拮抗薬であることがわかったが、[[molecular modeling/ja|分子モデリング]]を用いて、それらの構造はAng IIの[[pharmacophore/ja|ファーマコフォア]]をより忠実に[[mimic/ja|模倣]]しなければならないことがわかった。構造的な改良が加えられ，経口活性で強力な[[Ligand (biochemistry)/ja#Selective and non-selective|選択的]]非ペプチド性AT<sub>1</sub>受容体拮抗薬[[losartan/ja|ロサルタン]]が開発された。1995年にロサルタンは米国で臨床使用が承認され、それ以来さらに6種類のARBが承認されている。これらの薬物はその優れた[[Adverse effect (medicine)/ja|副作用]]プロファイルで知られており、[[clinical trials/ja|臨床試験]]では[[placebos/ja|プラセボ]]と同様であることが示されている。 |